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. 2013 Jan 16;19(1):7–17. doi: 10.2119/molmed.2012.00318

Table 2.

Competition affinities for different opioid receptors and ligands.

Receptor Ligand Ki (mean ± SEM) (nmol/L) % Displacement
dre-μ Met-ENK 684 ± 15 73.97 ± 1.29
Leu-ENK 1,317 ± 166 58.51 ± 2.68
β-END 186 ± 25 88.45 ± 2.03
MEGY 204 ± 53 78.98 ± 3.73
(d-Ala2)-MEGY 744 ± 27 66.72 ± 0.81
(d-Ala2, Val5)-MEGY 3,645 ± 621 43.16 ± 3.39
Morphine 187 ± 94 100
Naloxone 10.65 ± 1.53 100

Ki (nmol/L) Reference

dre-δ1 β-END 36.6 29
MEGY 427 21
Morphine 22 29
dre-δ2 Met-ENK 45 graphic file with name 12_318_gonzalez-nunezf7.jpg 30
Leu-ENK 175
MEGY 146 21
Morphine 1,400 30
rn-μa Met-ENK 1.80 graphic file with name 12_318_gonzalez-nunezf8.jpg 5
Leu-ENK 6.19
MERF 0.37
Morphine 7.48
rn-δb Met-ENK 0.45
Leu-ENK 0.37
MERF 0.57
Morphine 302
tg-μc Met-ENK 70.7 graphic file with name 12_318_gonzalez-nunezf9.jpg 32
Leu-ENK 117
β-END 55.9
tg-δc Met-ENK 24.9
Leu-ENK 198
β-END 284

This table summarizes the results obtained in competition binding assays (Ki and % displacement) using [3H]-diprenorphine on membrane homogenates from HEK293 cells that stably express the μ opioid receptor from zebrafish. The results of other competition binding studies for the zebrafish δ opioid receptors dre-δ1 and dre-δ2, prototypical mammalian δ and μ receptors rn-oprm1 (rn, Rattus norvegicus [rat]) and rn-oprm1 and the amphibian μ and δ receptors tg-oprm1 and tg-oprd1 (tg, Taricha granulosa [newt]) have also been included for comparison.

a

In this case, the radioligand used was the μ-selective peptidic analog [3H]-DAMGO and not [3H]-diprenorphine.

b

In this case, the radioligand used was the δ-selective peptidic analog [3H]-DPDPE and not [3H]-diprenorphine.

c

In this case, the radioligand used was the nonspecific antagonist [3H]-naloxone and not [3H]-diprenorphine.